在乙内酰脲部分和苯并咪唑支架之间具有基于疏水氨基酸连接子的纤溶酶抑制剂可增强抑制活性。
Plasmin inhibitors with hydrophobic amino acid-based linker between hydantoin moiety and benzimidazole scaffold enhance inhibitory activity.
作者信息
Teno Naoki, Gohda Keigo, Yamashita Yukiko, Otsubo Tadamune, Yamaguchi Masafumi, Wanaka Keiko, Tsuda Yuko
机构信息
Hiroshima International University, Faculty of Clinical Nutrition, 5-1-1, Hirokoshingai, Kure, Hiroshima 737-0112, Japan.
Computer-aided Molecular Modeling Research Center, Kansai (CAMM-Kansai), 3-32-302, Tsuto-Otsuka, Nishinomiya 663-8241, Japan.
出版信息
Bioorg Med Chem Lett. 2016 May 1;26(9):2259-61. doi: 10.1016/j.bmcl.2016.03.047. Epub 2016 Mar 15.
In this letter we report the design and synthesis of a series of plasmin inhibitors, which share the amino acid-based linker with limited free rotation between the hydantoin moiety and the benzimidazole scaffold. Our studies led to potent plasmin inhibitors and yielded important new insights into their structure-activity relationship for binding to the active site of plasmin.
在本信函中，我们报告了一系列纤溶酶抑制剂的设计与合成，这些抑制剂具有基于氨基酸的连接基团，在乙内酰脲部分与苯并咪唑支架之间具有有限的自由旋转。我们的研究得到了强效的纤溶酶抑制剂，并对它们与纤溶酶活性位点结合的构效关系产生了重要的新见解。
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